POTASSIUM AMINOSALICYLATE
Clinical safety rating
cautionComprehensive clinical and safety monograph for POTASSIUM AMINOSALICYLATE (POTASSIUM AMINOSALICYLATE).
Comprehensive clinical and safety monograph for POTASSIUM AMINOSALICYLATE (POTASSIUM AMINOSALICYLATE).
Adjunctive treatment of tuberculosis (as second-line agent)Off-label: treatment of ulcerative colitis (as mesalamine prodrug)
Exact mechanism unknown; may competitively inhibit folic acid synthesis and/or disrupt mycobacterial cell wall metabolism via inhibition of salicylate hydroxylation.
| Metabolism | Hepatic (acetylation to N-acetyl-4-aminosalicylic acid and other metabolites); also undergoes intestinal metabolism by gut bacteria. |
| Excretion | Renal: >80% as metabolites (acetyl, glycolyl conjugates) and unchanged drug; fecal: <5%. |
| Half-life | 0.5-1.5 hours for parent drug; acetylated metabolite half-life 2-3 hours; accumulation occurs in renal impairment. |
| Protein binding | 50-60% bound to albumin. |
| Volume of Distribution | 0.2-0.4 L/kg; reflects distribution into total body water with limited tissue penetration. |
| Bioavailability | Oral: ~90% absorbed; food may delay absorption. |
| Onset of Action | Oral: 2-4 weeks for bacteriostatic effect in tuberculosis; topical: not applicable. |
| Duration of Action | Dosing every 6-8 hours required due to rapid elimination; sustained effect requires consistent serum levels. |
| Molecular Weight | 191.3 |
Adults: 4 g (as granules or powder) orally twice daily, equivalent to 8 g/day of aminosalicylic acid base.
| Dosage form | POWDER |
| Renal impairment | GFR <50 mL/min: not recommended due to risk of accumulation; if unavoidable, reduce dose to 4 g once daily. GFR <30 mL/min: avoid use. |
| Liver impairment | Child-Pugh Class A: no adjustment. Child-Pugh Class B: reduce dose by 50% (to 2 g twice daily). Child-Pugh Class C: avoid use. |
| Pediatric use | Children: 200-300 mg aminosalicylic acid base per kg body weight per day, divided into 2 doses. Maximum 8 g/day. |
| Geriatric use | Start at lower end of dosing (4 g once daily) due to potential decreased renal function and increased risk of gastrointestinal intolerance. |
| 1st trimester | Insufficient human data; animal studies not available. Use only if clearly needed. |
| 2nd trimester | Limited data; no known teratogenic effects reported. Use only if benefit justifies risk. |
| 3rd trimester | Avoid near term due to potential for methemoglobinemia and hemolytic anemia in newborn. |
Clinical note
Comprehensive clinical and safety monograph for POTASSIUM AMINOSALICYLATE (POTASSIUM AMINOSALICYLATE).
| Placental transfer | Crosses placenta; fetal serum concentrations approximate maternal levels. |
| Breastfeeding | Minimal excretion into breast milk; levels considered low. Monitor infant for diarrhea or rash. Avoid in G6PD deficiency. |
| Lactation Rating | L3 - Moderately Safe |
| Teratogenic Risk | First trimester: Insufficient data; no known human teratogenicity but animal studies inconclusive. Second/third trimester: No documented fetal harm; use only if clearly needed. |
| Fetal Monitoring | Monitor serum potassium levels, renal function, and signs of GI intolerance. For fetus: ultrasound for growth and amniotic fluid volume. |
| Fertility Effects | No known effects on fertility in human studies. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
Hypersensitivity to aminosalicylatesSevere renal impairment (CrCl <30 mL/min)G6PD deficiency
| Precautions | Hypersensitivity reactions including fever and rash, Hepatotoxicity (discontinue if jaundice or liver enzyme elevation occurs), Renal impairment may require dose adjustment, Gastrointestinal intolerance, May cause hypocalcemia and hypokalemia, Interference with thyroid function tests |
| Food/Dietary | Avoid alcohol. Take with food or milk to reduce gastrointestinal irritation. Avoid large amounts of high-potassium foods (e.g., bananas, oranges, potatoes) unless directed by a physician, as this drug may alter potassium levels. No specific food restrictions beyond these. |
| Clinical Pearls | Monitor for hepatotoxicity, including elevated liver enzymes and bilirubin, especially in the first 3 months of therapy. Administer with food to reduce GI upset. Concurrent use with rifampin may decrease rifampin levels; separate doses by 8-12 hours. Contraindicated in severe renal impairment (CrCl < 30 mL/min) due to risk of hypokalemia and salicylate toxicity. Hypersensitivity reactions including fever, rash, and eosinophilia may occur; discontinue if severe. |
| Patient Advice | Take this medication with food or milk to prevent stomach upset. · Do not take antacids containing aluminum or magnesium within 3 hours of this medication. · Avoid alcohol while taking this medication due to increased risk of liver damage. · Report any signs of liver problems (yellowing skin or eyes, dark urine, abdominal pain) to your doctor immediately. · Use effective contraception during treatment as this drug may harm an unborn baby. · Do not stop taking this medication without consulting your doctor, even if you feel better. · Keep all appointments for blood tests to monitor liver function and potassium levels. |
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